Agomelatine (S-20098; BAN, rINN; Valdoxan, Melitor, Thymanax)

Description: Agomelatine (S20098; AGO-178; S-20098; AGO178; Valdoxan, Melitor, Thymanax) is a potent and specific agonist of MT1 and MT2 receptors with anti-depressive activity. It activates the isoforms of MT receptors such as CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2 with Kis of 0.1, 0.06, 0.12, and 0.27 nM, respectively. It is a unique antidepressant and is developed for treatment of major depressive disorder (MDD). It shows low affinities to cloned human 5-HT2A and 5-HT1A. In the in vivo studies, agomelatine causes increase of dopamine and noradrenaline levels via blocking the inhibitory input of 5-HT2C.